Zobrazeno 1 - 10
of 76
pro vyhledávání: '"Richard, Morphy"'
Autor:
Kristy Kikly, Howard Barff Broughton, William Chang, Selma Sapmaz, Richard Morphy, Holly A. Bina, Jim D. Durbin, Sherry Y Guo, Timothy Ivo Richardson, Jimmy P Steele, Ryan Edward Stites, Brian G. Getman, Vaught Grant Matthews, Veavi Ching-Yun Chang, Pamela K. Shetler, Greg L Durst, Denise D Edmondson, Rob Barr, Helene Rudyk, Charles Willis Lugar, Nita J. Patel, Christian Alexander Clarke, Kelly Wayne Furness, Nicole E New, David K. Clawson, Keith R. Stayrook, Mark Chambers, Brian Michael Mathes, Stephanie L. Stout, Wendy H. Gough
Publikováno v:
Journal of Medicinal Chemistry. 64:5470-5484
The Th17 pathway has been implicated in autoimmune diseases. The retinoic acid receptor-related orphan receptor C2 (RORγt) is a master regulator of Th17 cells and controls the expression of IL-17A. RORγt is expressed primarily in IL-17A-producing l
Autor:
Charles W, Lugar, Christian A, Clarke, Richard, Morphy, Helene, Rudyk, Selma, Sapmaz, Ryan E, Stites, Grant M, Vaught, Kelly, Furness, Howard B, Broughton, Greg L, Durst, David K, Clawson, Stephanie L, Stout, Sherry Y, Guo, Jim D, Durbin, Keith R, Stayrook, Denise D, Edmondson, Kristy, Kikly, Nicole E, New, Holly A, Bina, Mark G, Chambers, Pamela, Shetler, William Y, Chang, Veavi Ching-Yun, Chang, Rob, Barr, Wendy H, Gough, Jimmy P, Steele, Brian, Getman, Nita, Patel, Brian M, Mathes, Timothy I, Richardson
Publikováno v:
Journal of medicinal chemistry. 64(9)
The Th17 pathway has been implicated in autoimmune diseases. The retinoic acid receptor-related orphan receptor C2 (RORγt) is a master regulator of Th17 cells and controls the expression of IL-17A. RORγt is expressed primarily in IL-17A-producing l
Autor:
Véronique Gouverneur, John Richard Morphy, David M. H. Ascough, Gabriele Pupo, Robert S. Paton, Paolo Ricci, Kirsten E. Christensen, John M. Brown, Lukas Pfeifer, Francesco Ibba, Anna Chiara Vicini
Publikováno v:
Science
H-bond to deliver fluoride Simple fluoride salts are theoretically convenient reagents for carbon-fluorine bond formation. In practice, they are often insoluble in the solvents that dissolve their reaction partners. Pupo et al. developed urea-based c
Autor:
Tanatorn Khotavivattana, John Richard Morphy, Véronique Gouverneur, Maurice Médebielle, Paolo Ricci, Lukas Pfeifer
Publikováno v:
Chemical Science. 8:1195-1199
Alkenes substituted with a thiourea undergo C-CF3 followed by intramolecular C-S bond formation with the Togni reagent and trifluoroacetic acid (TFA) at room temperature; thiols and thioamides are not suitable S-sources for this reaction. This anti-a
Publikováno v:
In Tetrahedron 2003 59(12):2137-2145
Autor:
J. Richard Morphy
Publikováno v:
Attrition in the Pharmaceutical Industry: Reasons, Implications, and Pathways Forward
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7d673b5f15dde3aa9129e2c466c3d42c
https://doi.org/10.1002/9781118819586.ch8
https://doi.org/10.1002/9781118819586.ch8
Autor:
Jack Pick, Mark Craighead, Heather A. Zanetakos, Jeffrey J. Letourneau, Rachel Milne, Hema Desai, Leigh Campbell-Wan, Jeremy Presland, Michael Ohlmeyer, James R. Baker, Nasrin Ansari, Ray Jui-Hsiang Chan, Cliona P MacSweeney, Douglas S. Auld, Maria L. Webb, Jiuqiao Zhao, Chris Riviello, J. Richard Morphy, Stuart A. Best, Irina Neagu, Susan Elizabeth Napier, Koc-Kan Ho
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:3813-3817
Synthesis and structure–activity relationships (SAR) of a novel series of vasopressin V1b antagonists are described. 2-(6-Aminomethylaryl-2-aryl-4-oxo-quinazolin-3(4H)-yl)acetamide have been identified with low nanomolar affinity for the V1b recept
Autor:
Margaret Huggett, Sylviane Boucharens, Amanda J. Lyons, Ola Epemolu, Steven Laats, Lorcan Sherry, Mark York, Jos de Man, Richard Morphy, D. S. Fletcher, Peter C. Ray, Jane E. Wright, Philip Jones, Julia M. Adam, Brad Sherborne, Darcey Black, Nicole C.R. van Straten, Paul Westwood, Angus R. Brown
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:1084-1088
Rho kinase is an important target implicated in a variety of cardiovascular diseases. Herein, we report the optimisation of the fragment derived ATP-competitive ROCK inhibitors 1 and 2 into lead compound 14A. The initial goal of improving ROCK-I pote
Autor:
Anders Haunso, Richard Morphy, Julia M. Adam, Jos de Man, Ola Epemolu, Zoran Rankovic, Peter C. Ray, Sylviane Boucharens, Amanda J. Lyons, Jordi Mestres, Guido Z.R. Zaman, Lorcan Sherry, Angus R. Brown, Brad Sherborne, Jane E. Wright, Johnathan Bennett, Andrew J. Cook, Margaret Huggett, Philip Jones, Nicole C.R. van Straten, Steven Laats, Paul Westwood, Darcey Black, D. S. Fletcher
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:97-101
Fragment-based NMR screening of a small literature focused library led to identification of a historical thrombin/FactorXa building block, 17A, that was found to be a ROCK-I inhibitor. In the absence of an X-ray structure, fragment growth afforded 6-
Autor:
Dawn Buchanan, Joanna Passmore, Anders Haunsø, Matilda Bingham, Linsday Gibson, Margaret Huggett, Olaf Nimz, Richard Goodwin, Neil Andrew Dunbar, Susan Elizabeth Napier, Derek Angus, Richard Morphy, Andrea K. Houghton, Glenn Walker
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:271-275
Hit compound 1, a selective noradrenaline re-uptake transporter (NET) inhibitor was optimised to build in potency at the serotonin re-uptake transporter (SERT) whilst maintaining selectivity against the dopamine re-uptake transporter (DAT). During th